RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor.

RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor.

Bioorganic & medicinal chemistry letters (2011-08-20)

Andrei A Krysko, Georgiy V Samoylenko, Pavel G Polishchuk, Sergei A Andronati, Tatyana A Kabanova, Tetiana M Khristova, Victor E Kuz'min, Vladimir M Kabanov, Olga L Krysko, Alexandre A Varnek, Ruslan Ya Grygorash

PMID21852128

ABSTRAKT

The novel RGD mimetics with phthalimidine central fragment were synthesized with the use of 4-piperidine-4-yl-butyric, 4-piperidine-4-yl-benzoic, 4-piperazine-4-yl-benzoic and 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acids as surrogates of Arg motif. The synthesized compounds potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to α(IIb)β(3) integrin in a suspension of washed human platelets. The key α(IIb)β(3) protein-ligand interactions were determined in docking experiments.